Avitinib | B2995

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. It inhibits EGFR L858R/T790M double mutations with an IC₅₀ value of 0.18 nM which is nearly 43-fold potent over wild-type EGFR (IC₅₀ value of 7.68 nM) in kinase assays. In a xenograft model, oral administration at a daily dose of 500 mg/kg results in complete remission of tumors with EGFR-active and T790M mutations.

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. It inhibits EGFR L858R/T790M double mutations with an IC₅₀ value of 0.18 nM which is nearly 43-fold potent over wild-type EGFR (IC₅₀ value of 7.68 nM) in kinase assays. In a xenograft model, oral administration at a daily dose of 500 mg/kg results in complete remission of tumors with EGFR-active and T790M mutations.

B2995 | Avitinib DataSheet

Alternate Name/Synonyms: Abivertinib; N-[3-[[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]prop-2-enamide; N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; AC0010

Appearance: White to off-White Powder

Formulation:

CAS Number: 1557267-42-1

Structure Available?: True

Peptide sequence:

Salt Form: False

Molecular Formula: C₂₆H₂₆FN₇O₂

Molecular Weight: 487.53

Cell-Permeable?: False

Purity: >98%

Solubilities: ~30 mg/ml in DMSO, ethanol, DMF

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An irreversible EGFR inhibitor

MDL Number: MFCD29089376

PubChem CID: 72734520

SMILES: CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC4=C(C=CN4)C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)F

InChi: InChI=1S/C26H26FN7O2/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32)

InChi Key: UOFYSRZSLXWIQB-UHFFFAOYSA-N